Wellington Keri, Wagstaff Antona J
Adis International Limited, Auckland, New Zealand.
Drugs. 2003;63(13):1417-33. doi: 10.2165/00003495-200363130-00008.
Tranexamic acid (Transamin), Cyklokapron, Exacyl, Cyklo-f) is a synthetic lysine derivative that exerts its antifibrinolytic effect by reversibly blocking lysine binding sites on plasminogen and thus preventing fibrin degradation. In a number of small clinical studies in women with idiopathic menorrhagia, tranexamic acid 2-4.5 g/day for 4-7 days reduced menstrual blood loss by 34-59% over 2-3 cycles, significantly more so than placebo, mefenamic acid, flurbiprofen, etamsylate and oral luteal phase norethisterone at clinically relevant dosages. Intrauterine administration of levonorgestrel 20 microg/day, however, produced the greatest reduction (96% after 12 months) in blood loss; 44% of patients treated with levonorgestrel developed amenorrhoea. Tranexamic acid 1.5 g three times daily for 5 days also significantly reduced menstrual blood loss in women with intrauterine contraceptive device-associated menorrhagia compared with diclofenac sodium (150 mg in three divided doses on day 1 followed by 25 mg three times daily on days 2-5) or placebo. Tranexamic acid, mefenamic acid, etamsylate, flurbiprofen or diclofenac sodium had no effect on the duration of menses in the studies that reported such data. In a large noncomparative, nonblind, quality-of-life study, 81% of women were satisfied with tranexamic acid 3-6 g/day for 3-4 days/cycle for three cycles, and 94% judged their menstrual blood loss to be 'decreased' or 'strongly decreased' compared with untreated menstruations. The most commonly reported drug-related adverse events are gastrointestinal in nature. The total incidence of nausea, vomiting, diarrhoea and dyspepsia in a double-blind study was 12% in patients who received tranexamic acid 1g four times daily for 4 days for two cycles (not significantly different to the incidence in placebo recipients). In conclusion, the oral antifibrinolytic drug tranexamic acid is an effective and well tolerated treatment for idiopathic menorrhagia. In clinical trials, tranexamic acid was more effective at reducing menstrual blood loss than mefenamic acid, flurbiprofen, etamsylate and oral luteal phase norethisterone. Although it was not as effective as intrauterine administration of levonorgestrel, the high incidence of amenorrhoea and adverse events such as intermenstrual bleeding resulting from such treatment may be unacceptable to some patients. Comparative studies of tranexamic acid with epsilon - aminocaproic acid, danazol and combined oral contraceptives, as well as long-term tolerability studies, would help to further define the place of the drug in the treatment of menorrhagia. Nevertheless, tranexamic acid may be considered as a first-line treatment for the initial management of idiopathic menorrhagia, especially for patients in whom hormonal treatment is either not recommended or not wanted.
氨甲环酸（传明酸、凝血酸、Cyclokapron、Exacyl、Cyklo-f）是一种合成赖氨酸衍生物，通过可逆性阻断纤溶酶原上的赖氨酸结合位点发挥抗纤维蛋白溶解作用，从而防止纤维蛋白降解。在多项针对特发性月经过多女性的小型临床研究中，氨甲环酸2 - 4.5克/天，服用4 - 7天，在2 - 3个周期内可使月经失血减少34% - 59%，比安慰剂、甲芬那酸、氟比洛芬、氨甲苯酸和口服黄体期炔诺酮在临床相关剂量下减少的幅度显著更大。然而，宫内给予左炔诺孕酮20微克/天，失血减少幅度最大（12个月后为96%）；44%接受左炔诺孕酮治疗的患者出现闭经。与双氯芬酸钠（第1天150毫克分3次服用，随后第2 - 5天25毫克每日3次）或安慰剂相比，氨甲环酸1.5克每日3次服用5天，也能显著减少宫内节育器相关月经过多女性的月经失血。在报告了此类数据的研究中，氨甲环酸、甲芬那酸、氨甲苯酸、氟比洛芬或双氯芬酸钠对月经持续时间均无影响。在一项大型非对照、非盲法的生活质量研究中，81%的女性对氨甲环酸3 - 6克/天，每周期服用3 - 4天，共三个周期的治疗感到满意，与未治疗的月经相比，94%的女性认为她们的月经失血“减少”或“大幅减少”。最常报告的与药物相关的不良事件本质上是胃肠道方面的。在一项双盲研究中，接受氨甲环酸1克每日4次服用4天，共两个周期的患者中，恶心、呕吐、腹泻和消化不良的总发生率为12%（与接受安慰剂的患者发生率无显著差异）。总之，口服抗纤维蛋白溶解药物氨甲环酸是治疗特发性月经过多的一种有效且耐受性良好的疗法。在临床试验中，氨甲环酸在减少月经失血方面比甲芬那酸、氟比洛芬、氨甲苯酸和口服黄体期炔诺酮更有效。尽管它不如宫内给予左炔诺孕酮有效，但这种治疗导致的闭经高发生率以及诸如经间期出血等不良事件，可能对一些患者来说是不可接受的。氨甲环酸与ε - 氨基己酸、达那唑和复方口服避孕药的比较研究，以及长期耐受性研究，将有助于进一步明确该药物在月经过多治疗中的地位。然而，氨甲环酸可被视为特发性月经过多初始治疗的一线疗法，尤其是对于不推荐或不希望接受激素治疗的患者。
